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AntibioticsUpdate 2005 Cell Wall Synthesis Inhibitors Beta Lactams Penicillins (PCN) Cephalosporins Carbapenems Monobactams Vancomycin Bacitracin Polymyxin Beta Lactams B-lactams inhibit transpeptidase. Only effective against rapidly growing organisms that synthesize peptidoglycan. (Ineffective against mycobacteria.) The size, charge and hydrophobicity of the molecule determines the extent of its antibacterial activity. Penicillins Derived from Penicillium chrysogenum. PCN G and PCN V are unaltered products of Penicillium fermentation. Semi-synthetic penicillins are formed by addition of R groups to the main 6-aminopenicillanic acid ring. Adverse Reactions 5% of patients will develop a hypersensitivity reaction (penicilloic acid). Rashes - most common reaction. 50% do not have a recurrent rash. Ampicillin - rash in 50-100% of patients with mononucleosis. Adverse reactions Anaphylaxis – 1/10000 patients Hives, angioedema, rhinitis, asthma, and anaphylaxis. 10% mortality rate. Anaphylaxis possible after negative skin testing. Desensitization is an option if penicillin must be given. Avoid all other B-lactams. Natural Penicillins PCN G (IV/IM; $12/day) PCN V (Oral; $0.52/day) Active against Strep., peptostreptococcus, B anthracis, Actinomycosis, Corynebacterium, Listeria, Neisseria Treponema. Used for common oral infections. Anti-Staphylococcal Penicillins Methicillin, nafcillin, oxacillin, cloxacillin and dicloxacillin. Resist degradation by penicillinase. Useful for treating S. aureus. No added benefit in treating Strep. species. Methicillin is rarely used due to toxicity. Dicloxacillin ($0.87/day) - highest serum levels orally. Nafcillin ($15/day) - preferred parenteral drug. Aminopenicillins Ampicillin (IV; $1.95/day) Ampicillin/sulbactam (Unasyn; IV; $30.76/day) Amoxicillin (Oral; $0.32/day). Amoxicillin/clavulanate (Augmentin; $6.63/day) Sulbactam and clavulanic acid increase activity against B-lactamase producing organisms. Extended antimicrobial
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